Novel nucleotide analogues as potential substrates for TMPK, a key enzyme in the metabolism of AZT |
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Authors: | Müller H C Meier C Balzarini J Reinstein J |
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Affiliation: | Institute of Organic Chemistry, University of Hamburg, Hamburg, Germany. |
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Abstract: | Novel cyclic and acyclic analogues of dTMP and AZTMP were synthesized from the corresponding cycloSal-phosphotriesters. This method yielded the nucleotides in good yields with a simple work-up. Investigation of the substrate properties of the modified nucleotides towards TmpK showed, that they are very poor substrates for this key enzyme in the bioactivation of AZT. |
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